Search Results - "WEBB, Robert R"
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A calcineurin antifungal strategy with analogs of FK506
Published in Bioorganic & medicinal chemistry letters (01-06-2017)“…[Display omitted] A novel antifungal strategy targeting the inhibition of calcineurin is described. To develop a calcineurin based inhibitor of pathogenic…”
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Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity
Published in Bioorganic & medicinal chemistry letters (01-03-2005)Get full text
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A new family of H3 receptor antagonists based on the natural product Conessine
Published in Bioorganic & medicinal chemistry letters (15-02-2008)“…A new family of Histamine H(3) receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H(3) antagonist…”
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Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity
Published in Journal of medicinal chemistry (24-01-2008)“…The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more…”
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Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1
Published in Bioorganic & medicinal chemistry letters (08-04-2002)“…We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These…”
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Discovery and Structure−Activity Relationship of 3-Methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Published in Journal of medicinal chemistry (10-06-2010)“…Serotonin, which is stored in platelets and is released during thrombosis, activates platelets via the 5-HT2A receptor. 5-HT2A receptor inverse agonists thus…”
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Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (15-09-2009)Get full text
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Synthesis of a tetramethyl analog of teleocidin
Published in Journal of organic chemistry (01-07-1991)Get full text
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Alkaloid synthesis via intramolecular ene reactions. 1. Application to (.+-.)-crinane
Published in Journal of the American Chemical Society (01-06-1981)Get full text
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Alkaloid synthesis via intramolecular ene reaction. 2. Application to dl-mesembrine and dl-dihydromaritidine
Published in Journal of organic chemistry (01-03-1982)Get full text
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Discovery and SAR of new benzazepines as potent and selective 5-HT 2C receptor agonists for the treatment of obesity
Published in Bioorganic & medicinal chemistry letters (01-03-2005)“…The synthesis and SAR of a 3-benzazepine series of selective 5-HT 2C agonists is described. We report on the synthesis, biological evaluation and…”
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A new family of H 3 receptor antagonists based on the natural product Conessine
Published in Bioorganic & medicinal chemistry letters (15-02-2008)“…A new family of Histamine H 3 receptor antagonists ( 5a– t) has been prepared based on the structure of the natural product Conessine, a known H 3 antagonist…”
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15
Lewis acid catalyzed cyclocondensations of formaldehyde with activated dienes. A direct route to pyranosidal pentoses
Published in Journal of organic chemistry (01-06-1984)Get full text
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Synthesis and antiviral activity of the nucleotide analog (S)-1-[3-hydroxy-2-(phosphonylmethoxy)propyl]cystosine
Published in Journal of medicinal chemistry (01-07-1989)Get full text
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Discovery and Structure−Activity Relationship of 3-Methoxy- N -(3-(1-methyl-1 H -pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine 2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Published in Journal of medicinal chemistry (10-06-2010)Get full text
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Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2A Inverse Agonists for the Treatment of Insomnia
Published in Journal of medicinal chemistry (11-03-2010)“…Insomnia affects a growing portion of the adult population in the U.S. Most current therapeutic approaches to insomnia primarily address sleep onset latency…”
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Solubilized phenyl-pyrazole ureas as potent, selective 5-HT sub(2A) inverse-agonists and their application as antiplatelet agents
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…Potent 5-HT sub(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in…”
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